Antibacterial Multi-Layered Nanocellulose-Based Patches Loaded with Dexpanthenol for Wound Healing Applications

Antibacterial multi-layered patches composed of an oxidized bacterial cellulose (OBC) membrane loaded with dexpanthenol (DEX) and coated with several chitosan (CH) and alginate (ALG) layers were fabricated by spin-assisted layer-by-layer (LbL) assembly. Four patches with a distinct number of layers (5, 11, 17, and 21) were prepared. These nanostructured multi-layered patches reveal a thermal stability up to 200 °C, high mechanical performance (Young’s modulus ≥ 4 GPa), and good moisture-uptake capacity (240–250%). Moreover, they inhibited the growth of the skin pathogen Staphylococcus aureus (3.2–log CFU mL−1 reduction) and were non-cytotoxic to human keratinocytes (HaCaT cells). The in vitro release profile of DEX was prolonged with the increasing number of layers, and the time-dependent data imply a diffusion/swelling-controlled drug release mechanism. In addition, the in vitro wound healing assay demonstrated a good cell migration capacity, headed to a complete gap closure after 24 h. These results certify the potential of these multi-layered polysaccharides-based patches toward their application in wound healing.

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Nanocellulose-Based Patches Loaded with Hyaluronic Acid and Diclofenac towards Aphthous Stomatitis Treatment

Nanomaterials ◽

10.3390/nano10040628 ◽

2020 ◽

Vol 10 (4) ◽

pp. 628 ◽

Cited By ~ 3

Author(s):

João P. F. Carvalho ◽

Ana C. Q. Silva ◽

Verónica Bastos ◽

Helena Oliveira ◽

Ricardo J. B. Pinto ◽

...

Keyword(s):

Hyaluronic Acid ◽

In Vitro Release ◽

Three Dimensional ◽

Human Keratinocytes ◽

Controlled Drug Release ◽

Dynamic Mechanical Properties ◽

Aphthous Stomatitis ◽

Release Mechanism ◽

Porous Network

Nanostructured patches composed of bacterial nanocellulose (BNC), hyaluronic acid (HA) and diclofenac (DCF) were developed, envisioning the treatment of aphthous stomatitis. Freestanding patches were prepared via diffusion of aqueous solutions of HA and DCF, with different concentrations of DCF, into the wet BNC three-dimensional porous network. The resultant dual polysaccharides-based patches with a nanostructured morphology present thermal stability up to 200 °C, as well as good dynamic mechanical properties, with a storage modulus higher than 1.0 GPa. In addition, the patches are non-cytotoxic to human keratinocytes (HaCaT cells), with a cell viability of almost 100% after 24 h. The in vitro release profile of DCF from the patches was evaluated in simulated saliva, and the data refer to a diffusion- and swelling-controlled drug-release mechanism. The attained results hint at the possibility of using these dual polysaccharides-based oral mucosal patches to target aphthous stomatitis.

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FABRICATION OF NANO CLAY INTERCALATED POLYMERIC MICROBEADS FOR CONTROLLED RELEASE OF CURCUMIN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i1.39965 ◽

2021 ◽

pp. 206-215

Author(s):

DHARMENDER PALLERLA ◽

SUMAN BANOTH ◽

SUNKARI JYOTHI

Keyword(s):

Drug Release ◽

In Vitro Release ◽

Controlled Drug Release ◽

Fickian Diffusion ◽

Simulated Gastric Fluid ◽

Release Mechanism ◽

Release Studies ◽

Swelling Studies ◽

Vitro Release

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.

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Synthesis and Characterization of Lyophilized Chitosan-Based Hydrogels Cross-Linked with Benzaldehyde for Controlled Drug Release

Journal of Chemistry ◽

10.1155/2020/8747639 ◽

2020 ◽

Vol 2020 ◽

pp. 1-10 ◽

Cited By ~ 1

Author(s):

Fouad Damiri ◽

Yahya Bachra ◽

Chaimaa Bounacir ◽

Asmae Laaraibi ◽

Mohammed Berrada

Keyword(s):

Ascorbic Acid ◽

Drug Release ◽

Drug Loading ◽

In Vitro Release ◽

Controlled Drug Release ◽

Tween 20 ◽

Release Mechanism ◽

Synthetic Process ◽

Chitosan Salt

In this study, chitosan-based hydrogels were produced by incorporating three drugs with a different solubility into a polymer matrix. The lyophilized chitosan salt was prepared using an innovative and less-expensive synthetic process by the freeze-drying technique. Firstly, the three drugs (caffeine, ascorbic acid, and 5-fluorouracil (5-FU)) were selected as model drugs to test the in vitro release behavior of the hydrogel. The drugs were solubilized in chitosan salt, lyophilized, and cross-linked with benzaldehyde involving the formation of a Schiff base with (–C=N-) linkage to produce a physical hydrogel. Subsequently, the physicochemical properties of N-benzyl chitosan and lyophilized chitosan salt were evaluated by Fourier-transform infrared (FTIR) spectra, scanning electron microscopy (SEM), and thermogravimetric analysis (TGA). The intrinsic viscosity of the conventional chitosan was determined by the Mark–Houwink–Sakurada equation. Moreover, the kinetics of hydrogel swelling and drug release were studied by the UV-visible method at physiological conditions (pH = 7.4 at 37°C). The results show that lyophilized N-benzyl chitosan had a maximum swelling ratio of 720 ± 2% by immersion in phosphate-buffered saline solutions (PBS) (pH = 7.4 at 37°C). In vitro drug releases were evaluated in PBS, and the obtained results show that the maximum drug release after 24 h was 42% for caffeine, 99% for 5-FU, and 94% for ascorbic acid. Then, to optimize the cumulative release of caffeine, Tween 20 was added and 98% as a release percentage was obtained. The drug-loading results were investigated with the Korsmeyer–Peppas kinetic model and applied to determine the drug release mechanism.

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Controlled Drug Release Formulation by Sequential Crosslinking of Multilayered Electrospun Gelatin Nanofiber Mat

MRS Advances ◽

10.1557/adv.2016.320 ◽

2016 ◽

Vol 1 (29) ◽

pp. 2107-2113 ◽

Cited By ~ 3

Author(s):

Anindita Laha ◽

Saptarshi Majumdar ◽

Chandra S Sharma

Keyword(s):

Drug Release ◽

Drug Stability ◽

Single Layer ◽

Controlled Drug Release ◽

Release Mechanism ◽

Layer By Layer ◽

Drug Release Profile ◽

Release Formulation ◽

Electrospun Gelatin

ABSTRACTThe major aim of the present study is to develop and explore the potential of large surface area electrospun polymer nanofabric as a carrier for controlled and sustained release, in particular for hydrophobic drugs. Gelatin (type A), FDA approved natural polymer was electrospun in a mixture of solvent (20% acetic acid in water) to yield long, continuous and uniform fibers with average diameter ∼ 200 nm. Piperine was chosen as a model hydrophobic drug in this study. As gelatin is highly soluble in aqueous medium, we crosslinked electrospun gelatin nanofibers using saturated GTA vapor to increase the water resistive properties. For controlled release over a period of 12 h, we devised several strategies to vary the crosslinking conditions and accordingly understand their effect on drug release mechanism. One of such successful efforts was based on deposition of multiple layers of electrospun fabric by sandwiching between drug loaded gelatin nanofibers and without drug gelatin nanofibers from both sides. Not only the layer by layer deposition, we also crosslinked the different layer in the same sequential way. Sequential crosslinking using GTA vapor in different layers of the fabric, helped in uniform crosslinking throughout the thickness compared to crosslinking after final deposition in the form of a single layer. Effect of different crosslinking strategies was investigated in terms of surface morphology and drug stability. Finally,in-vitrorelease study was performed maintaining the physiological conditions mimicking GI tract to analyze the effect of crosslinking on the drug release profile. Thein-vitrostudies concluded that the controlled drug release can be achieved by tuning the thickness of individual fabric layer followed by their sequential crosslinking, which finally affects the diffusional barrier for drug release. Interestingly, we also found that only 6 min exposure to saturated GTA vapor is sufficient to provide the required drug release in contrast to up to 24 h as reported in literature. This finding also addresses the toxicity problem associated with the use of GTA as a cross-linker.

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Development of a Topical Insulin Polymeric Nanoformulation for Skin Burn Regeneration: An Experimental Approach

International Journal of Molecular Sciences ◽

10.3390/ijms22084087 ◽

2021 ◽

Vol 22 (8) ◽

pp. 4087

Author(s):

Maria Quitério ◽

Sandra Simões ◽

Andreia Ascenso ◽

Manuela Carvalheiro ◽

Ana Paula Leandro ◽

...

Keyword(s):

Wound Healing ◽

Healing Process ◽

In Vitro Release ◽

Peptide Hormone ◽

Plga Nanoparticles ◽

Wound Healing Process ◽

Target Area ◽

Encapsulation Process

Insulin is a peptide hormone with many physiological functions, besides its use in diabetes treatment. An important role of insulin is related to the wound healing process—however, insulin itself is too sensitive to the external environment requiring the protective of a nanocarrier. Polymer-based nanoparticles can protect, deliver, and retain the protein in the target area. This study aims to produce and characterize a topical treatment for wound healing consisting of insulin-loaded poly-DL-lactide/glycolide (PLGA) nanoparticles. Insulin-loaded nanoparticles present a mean size of approximately 500 nm and neutral surface charge. Spherical shaped nanoparticles are observed by scanning electron microscopy and confirmed by atomic force microscopy. SDS-PAGE and circular dichroism analysis demonstrated that insulin preserved its integrity and secondary structure after the encapsulation process. In vitro release studies suggested a controlled release profile. Safety of the formulation was confirmed using cell lines, and cell viability was concentration and time-dependent. Preliminary safety in vivo assays also revealed promising results.

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Dexamethasone-Loaded Lipomers: Development, Characterization, and Skin Biodistribution Studies

Pharmaceutics ◽

10.3390/pharmaceutics13040533 ◽

2021 ◽

Vol 13 (4) ◽

pp. 533

Author(s):

Eloy Pena-Rodríguez ◽

Maria Lajarin-Reinares ◽

Aida Mata-Ventosa ◽

Sandra Pérez-Torras ◽

Francisco Fernández-Campos

Keyword(s):

In Vitro Release ◽

Human Keratinocytes ◽

Topical Administration ◽

In Vitro Cytotoxicity ◽

Hair Follicles ◽

Vertical Diffusion ◽

Biodistribution Studies ◽

Follicular Targeting ◽

Depot Effect

Follicular targeting has gained more attention in recent decades, due to the possibility of obtaining a depot effect in topical administration and its potential as a tool to treat hair follicle-related diseases. Lipid core ethyl cellulose lipomers were developed and optimized, following which characterization of their physicochemical properties was carried out. Dexamethasone was encapsulated in the lipomers (size, 115 nm; polydispersity, 0.24; zeta-potential (Z-potential), +30 mV) and their in vitro release profiles against dexamethasone in solution were investigated by vertical diffusion Franz cells. The skin biodistribution of the fluorescent-loaded lipomers was observed using confocal microscopy, demonstrating the accumulation of both lipomers and fluorochromes in the hair follicles of pig skin. To confirm this fact, immunofluorescence of the dexamethasone-loaded lipomers was carried out in pig hair follicles. The anti-inflammatory (via TNFα) efficacy of the dexamethasone-loaded lipomers was demonstrated in vitro in an HEK001 human keratinocytes cell culture and the in vitro cytotoxicity of the nanoformulation was investigated.

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Development and Evaluation of Rifampicin Loaded Alginate–Gelatin Biocomposite Microfibers

Polymers ◽

10.3390/polym13091514 ◽

2021 ◽

Vol 13 (9) ◽

pp. 1514

Author(s):

Ameya Sharma ◽

Vivek Puri ◽

Pradeep Kumar ◽

Inderbir Singh ◽

Kampanart Huanbutta

Keyword(s):

Wound Healing ◽

Xanthan Gum ◽

In Vitro Release ◽

Antimicrobial Properties ◽

Entrapment Efficiency ◽

Tissue Proliferation ◽

Naturally Occurring ◽

Reinforcing Material ◽

Vitro Release

Various systematic phases such as inflammation, tissue proliferation, and phases of remodeling characterize the process of wound healing. The natural matrix system is suggested to maintain and escalate these phases, and for that, microfibers were fabricated employing naturally occurring polymers (biopolymers) such as sodium alginate, gelatin and xanthan gum, and reinforcing material such as nanoclay was selected. The fabrication of fibers was executed with the aid of extrusion-gelation method. Rifampicin, an antibiotic, has been incorporated into a biopolymeric solution. RF1, RF2, RF3, RF4 and RF5 were coded as various formulation batches of microfibers. The microfibers were further characterized by different techniques such as SEM, DSC, XRD, and FTIR. Mechanical properties and physical evaluations such as entrapment efficiency, water uptake and in vitro release were also carried out to explain the comparative understanding of the formulation developed. The antimicrobial activity and whole blood clotting of fabricated fibers were additionally executed, hence they showed significant results, having excellent antimicrobial properties; they could be prominent carriers for wound healing applications.

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Development of Spanish Broom and Flax Dressings with Glycyrrhetinic Acid-Loaded Films for Wound Healing: Characterization and Evaluation of Biological Properties

Pharmaceutics ◽

10.3390/pharmaceutics13081192 ◽

2021 ◽

Vol 13 (8) ◽

pp. 1192

Author(s):

Angela Abruzzo ◽

Concettina Cappadone ◽

Valentina Sallustio ◽

Giovanna Picone ◽

Martina Rossi ◽

...

Keyword(s):

Wound Healing ◽

Drug Loading ◽

Healing Process ◽

In Vitro Release ◽

Sodium Hyaluronate ◽

Biological Properties ◽

Glycyrrhetinic Acid ◽

Wound Dressings ◽

Biological Studies

The selection of an appropriate dressing for each type of wound is a very important procedure for a faster and more accurate healing process. So, the aim of this study was to develop innovative Spanish Broom and flax wound dressings, as alternatives to cotton used as control, with polymeric films containing glycyrrhetinic acid (GA) to promote wound-exudate absorption and the healing process. The different wound dressings were prepared by a solvent casting method, and characterized in terms of drug loading, water uptake, and in vitro release. Moreover, biological studies were performed to evaluate their biocompatibility and wound-healing efficacy. Comparing the developed wound dressings, Spanish Broom dressings with GA-loaded sodium hyaluronate film had the best functional properties, in terms of hydration ability and GA release. Moreover, they showed a good biocompatibility, determining a moderate induction of cell proliferation and no cytotoxicity. In addition, the wound-healing test revealed that the Spanish Broom dressings promoted cell migration, further facilitating the closure of the wound.

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Achyrocline satureioides (Lam.) DC (Asteraceae) Extract-Loaded Nanoemulsions as a Promising Topical Wound Healing Delivery System: In Vitro Assessments in Human Keratinocytes (HaCaT) and HET-CAM Irritant Potential

Pharmaceutics ◽

10.3390/pharmaceutics13081241 ◽

2021 ◽

Vol 13 (8) ◽

pp. 1241

Author(s):

Lucélia Albarello Balestrin ◽

Tainá Kreutz ◽

Flávia Nathiely Silveira Fachel ◽

Juliana Bidone ◽

Nicolly Espindola Gelsleichter ◽

...

Keyword(s):

Wound Healing ◽

Hacat Cell ◽

Chorioallantoic Membrane ◽

Human Keratinocytes ◽

Scratch Assay ◽

Hen’S Egg ◽

And Migration ◽

Achyrocline Satureioides ◽

Proliferation And Migration

Achyrocline satureioides (Lam.) DC Asteraceae extracts (ASEs) have been investigated for the treatment of various skin disorders. This study reports the effects of ASE-loaded nanoemulsions (NEASE) on the cellular viability, death by necrosis, and migration of immortalized human keratinocytes (HaCaT cell line), as well as the irritant potential through the hen’s egg chorioallantoic membrane test (HET-CAM). NEASE exhibited a polydispersity index above 0.12, with a droplet size of 300 nm, ζ-potential of −40 mV, and content of flavonoids close to 1 mg/mL. No cytotoxicity of the ASE was observed on HaCaT by MTT assay (up to 10 µg/mL). A significant increase of HaCaT viability was observed to NEASE (up to 5 μg/mL of flavonoids), compared to treatment with the ASE. The necrosis death evaluation demonstrated that only NEASE did not lead to cell death at all the tested concentrations. The scratch assay demonstrated that NEASE was able to increase the cell migration at low flavonoid concentrations. Finally, the HET-CAM test proved the non-irritative potential of NEASE. Overall, the results indicate the potential of the proposed formulations for topical use in wound healing, in view of their promising effects on proliferation and migration in keratinocytes, combined with an indication of the absence of cytotoxicity and non-irritating potential.

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DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

Journal of Biomedical and Pharmaceutical Research ◽

10.32553/jbpr.v7i6.559 ◽

2018 ◽

Vol 7 (6) ◽

Author(s):

Mohini Sihare ◽

Rajendra Chouksey

Keyword(s):

Drug Release ◽

Release Kinetics ◽

In Vitro Release ◽

Release Profile ◽

Matrix Tablets ◽

In Vivo Studies ◽

Release Mechanism ◽

In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

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